Zaleplon

Indications and usage: Zaleplon is indicated for the short-term treatment of insomnia. Zaleplon has been shown to decrease the time to sleep onset for up to 30 days in controlled clinical studies . It has not been shown to increase total sleep time or decrease the number of awakenings. The clinical trials performed in support of efficacy ranged from a single night to 5 weeks in duration. The final formal assessments of sleep latency were performed at the end of treatment.

CLINICAL PHARMACOLOGY Pharmacodynamics and Mechanism of Action While zaleplon is a hypnotic agent with a chemical structure unrelated to benzodiazepines, barbiturates, or other drugs with known hypnotic properties, it interacts with the gamma-aminobutyric acid-benzodiazepine (GABA-BZ) receptor complex. Subunit modulation of the GABA-BZ receptor chloride channel macromolecular complex is hypothesized to be responsible for some of the pharmacological properties of benzodiazepines, which include sedative, anxiolytic, muscle relaxant, and anticonvulsive effects in animal models.

Following administration (5 mg/1 Capsule), Zaleplon achieves Approximately 65% to 77% enteral uptake across labeled Zaleplon strengths bioavailability and maximum serum exposure occurs 2–3 hours after zaleplon dosing onset, governed by a Steady-state plasma equilibrium reached over 9–22 hour t½ intervals for Zaleplon terminal half-life through predominantly hepatic biotransformation with renal elimination of polar zaleplon conjugates.

Before initiating Zaleplon at 5 mg/1 Capsule, clinical safety checklists rule out contraindications zalepon is contraindicated in patients:; who have experienced complex sleep behaviors after taking zaleplon .; with hypersensitivity to zaleplon or any excipients in the formulation .. Logged tolerability patterns center on nausea (8.2% of reports), headache (6.9% of reports), dizziness (6.1% of reports).